No evidence for functional involvement of 5-HT2B receptors in serotonin-induced vasodilatation in the human forearm.
No evidence for functional involvement of 5-HT2B receptors in serotonin-induced vasodilatation in the human forearm.
复制标题
没有证据表明 5-HT2B 受体在人体前臂中血清素诱导的血管舒张中发挥功能作用。
DOI：
10.1097/00005344-200012000-00003
复制
发表时间：
2000
影响因子：
3
通讯作者：
G. Blauw
中科院分区：
文献类型：
--
作者：
M. Kemme;J. Burggraaf;R. Schoemaker;A. Cohen;G. Blauw
参与5-羟色胺（5-HT）诱导的人前臂血管舒张的受体尚未确定。实验数据指向位于内皮上的5-HT 2B受体。RS-127445（2-氨基-4-（4-氟萘-1-基）-6-异丙基嘧啶）是一种新型强效和选择性5-HT 2B受体拮抗剂。在一项在6名健康志愿者中进行的双盲、随机化、安慰剂对照、交叉研究中，研究了口服RS-127445（500 mg）对5-HT诱导的血管舒张的影响。在每个研究日，在给药前和经口摄入后20、65、110、230和470 min，将5-HT（0.5 ng/kg/min）输注至肱动脉8 min。在每次输注时，采集用于研究药物测定的血浆样品，并使用静脉闭塞体积描记法评估前臂血流。尽管（log）药物浓度超过pKi，但RS-127445浓度与5-HT诱导的血管舒张之间无相关性。5-HT诱导的血管舒张在治疗和时间点之间没有差异。似乎在人前臂中5-HT介导的血管舒张中没有5-HT 2B受体的功能参与。
The receptor involved in the serotonin (5-hydroxytryptamine [5-HT])-induced vasodilatation in the human forearm has not yet been identified. Experimental data point to the 5-HT2B receptor located on the endothelium. RS-127445 (2-amino-4-(4-fluoronaphthyl-1-yl)-6-isopropylpyrimidine) is a novel potent and selective 5-HT2B receptor antagonist. The effect of oral RS-127445 (500 mg) on 5-HT-induced vasodilatation was studied in a double-blind, randomized, placebo-controlled, crossover study in six healthy volunteers. On each study day 5-HT (0.5 ng/kg/min) was infused into the brachial artery for 8 min, before drug administration and at intervals of 20, 65, 110, 230, and 470 min after oral ingestion. At each infusion, plasma samples for study drug assay were taken and forearm blood flow was assessed using venous occlusion plethysmography. Although (log) drug concentrations exceeded pKi, there was no correlation between RS-127445 concentrations and 5-HT-induced vasodilatation. 5-HT-induced vasodilatation did not differ between treatments and time points. It appears that there is no functional involvement of 5-HT2B receptors in 5-HT-mediated vasodilatation in the human forearm.